2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide as selective glycine antagonist with in vivo activity.
2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the effectiveness of glycine antagonists in vivo.
Micheli
F
F
GlaxoWellcome S.p.A., Medicines Research Center, Verona, Italy. fm20244@ggr.co.uk
Cugola
A
A
Donati
D
D
Missio
A
A
Pecunioso
A
A
Reggiani
A
A
Tarzia
G
G
D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D001665:Binding Sites / Q000187:drug effects; D003497:Cyclic N-Oxides / Q000138:chemical synthesis / Q000494:pharmacology*; D016291:Dizocilpine Maleate / Q000494:pharmacology; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology; D005998:Glycine / Q000037:antagonists & inhibitors* / Q000187:drug effects; D007736:Kynurenic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D016202:N-Methylaspartate; D018696:Neuroprotective Agents / Q000494:pharmacology*; D011719:Pyrazines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000517:prevention & control; D013239:Stereotyped Behavior / Q000187:drug effects; D013331:Strychnine / Q000494:pharmacology
C111196:2,3-dihydro-6,7-dichloropyrido(2,3-b)pyrazine-8-oxide; D003497:Cyclic N-Oxides; D018691:Excitatory Amino Acid Antagonists; D018696:Neuroprotective Agents; D011719:Pyrazines; D016194:Receptors, N-Methyl-D-Aspartate; D016202:N-Methylaspartate; D016291:Dizocilpine Maleate; D007736:Kynurenic Acid; D013331:Strychnine; C057013:7-chlorokynurenic acid; D005998:Glycine